CN105229002A - 抑制bet蛋白的二氢吡啶并吡嗪酮 - Google Patents

抑制bet蛋白的二氢吡啶并吡嗪酮 Download PDF

Info

Publication number
CN105229002A
CN105229002A CN201380073359.5A CN201380073359A CN105229002A CN 105229002 A CN105229002 A CN 105229002A CN 201380073359 A CN201380073359 A CN 201380073359A CN 105229002 A CN105229002 A CN 105229002A
Authority
CN
China
Prior art keywords
base
dimethyl
pyrazine
amino
oxo
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Pending
Application number
CN201380073359.5A
Other languages
English (en)
Chinese (zh)
Inventor
N·施梅斯
B·贝德
B·海德勒
D·斯托茨基
P·勒热纳
A·E·费尔南德兹-蒙塔拉瓦
T·斯特菲尔德
D·加伦坎普
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Bayer Pharma AG
Original Assignee
Bayer Pharma AG
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Bayer Pharma AG filed Critical Bayer Pharma AG
Publication of CN105229002A publication Critical patent/CN105229002A/zh
Pending legal-status Critical Current

Links

Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/16—Masculine contraceptives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D493/00—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system
    • C07D493/02—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system in which the condensed system contains two hetero rings
    • C07D493/10—Spiro-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/10—Spiro-condensed systems

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Epidemiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Pain & Pain Management (AREA)
  • Urology & Nephrology (AREA)
  • Oncology (AREA)
  • Rheumatology (AREA)
  • Communicable Diseases (AREA)
  • Hospice & Palliative Care (AREA)
  • Virology (AREA)
  • Immunology (AREA)
  • Psychiatry (AREA)
  • Vascular Medicine (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Peptides Or Proteins (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
CN201380073359.5A 2012-12-20 2013-12-17 抑制bet蛋白的二氢吡啶并吡嗪酮 Pending CN105229002A (zh)

Applications Claiming Priority (7)

Application Number Priority Date Filing Date Title
EP12198623 2012-12-20
EP12198623.6 2012-12-20
EP13182252 2013-08-29
EP13182252.0 2013-08-29
EP13191933.4 2013-11-07
EP13191933 2013-11-07
PCT/EP2013/076784 WO2014095774A1 (de) 2012-12-20 2013-12-17 Bet-proteininhibitorische dihydropyridopyrazinone

Publications (1)

Publication Number Publication Date
CN105229002A true CN105229002A (zh) 2016-01-06

Family

ID=49779903

Family Applications (1)

Application Number Title Priority Date Filing Date
CN201380073359.5A Pending CN105229002A (zh) 2012-12-20 2013-12-17 抑制bet蛋白的二氢吡啶并吡嗪酮

Country Status (10)

Country Link
US (1) US20160193206A1 (de)
EP (1) EP2935260A1 (de)
JP (1) JP2016504990A (de)
CN (1) CN105229002A (de)
AR (1) AR094148A1 (de)
CA (1) CA2895404A1 (de)
HK (1) HK1213899A1 (de)
TW (1) TW201427981A (de)
UY (1) UY35205A (de)
WO (1) WO2014095774A1 (de)

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN109350616A (zh) * 2018-12-18 2019-02-19 南华大学 I-brd9或其衍生物在制备抗癫痫药物中的应用
CN113717080A (zh) * 2021-10-09 2021-11-30 西安瑞联新材料股份有限公司 一种4-氯-2-氰基苯磺酰氯的合成方法

Families Citing this family (34)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN105229002A (zh) * 2012-12-20 2016-01-06 拜耳医药股份有限公司 抑制bet蛋白的二氢吡啶并吡嗪酮
EP2970282B1 (de) 2013-03-15 2019-08-21 Incyte Holdings Corporation Tricyclische heterocyclen als bet-proteininhibitoren
ES2635560T3 (es) 2013-07-08 2017-10-04 Incyte Holdings Corporation Heterociclos tricíclicos como inhibidores de la proteína NET
US20160176867A1 (en) * 2013-07-09 2016-06-23 Bayer Pharma Aktiengesellschaft Modified bet-protein-inhibiting dihydroquinoxalinones and dihydropyridopyrazinones
RU2016105108A (ru) 2013-07-25 2017-08-30 Дана-Фарбер Кэнсер Инститьют, Инк. Ингибиторы факторов транскрипции и их применение
WO2015081189A1 (en) 2013-11-26 2015-06-04 Incyte Corporation Bicyclic heterocycles as bet protein inhibitors
US9399640B2 (en) 2013-11-26 2016-07-26 Incyte Corporation Substituted pyrrolo[2,3-c]pyridines and pyrazolo[3,4-c]pyridines as BET protein inhibitors
WO2015095492A1 (en) 2013-12-19 2015-06-25 Incyte Corporation Tricyclic heterocycles as bet protein inhibitors
KR20160111520A (ko) * 2014-01-31 2016-09-26 다나-파버 캔서 인스티튜트 인크. 디히드로프테리디논 유도체 및 그의 용도
JP2017504651A (ja) 2014-01-31 2017-02-09 ダナ−ファーバー キャンサー インスティテュート， インコーポレイテッド ジアゼパン誘導体の使用
KR20160115953A (ko) 2014-01-31 2016-10-06 다나-파버 캔서 인스티튜트 인크. 디아미노피리미딘 벤젠술폰 유도체 및 그의 용도
CN106414442B (zh) 2014-04-23 2019-03-15 因赛特公司 作为BET蛋白抑制剂的1H-吡咯并[2,3-c]吡啶-7(6H)-酮和吡唑并[3,4-c]吡啶-7(6H)-酮
US20170121322A1 (en) * 2014-06-18 2017-05-04 Bayer Pharma Aktiengesellschaft Bet-protein inhibiting 3,4-dihydropyrido[2,3-b]pyrazinones with meta-substituted aromatic amino- or ether groups
WO2015193217A1 (de) * 2014-06-18 2015-12-23 Bayer Pharma Aktiengesellschaft Bet-proteininhibitorische dihydropyrido[2,3-b]pyrazinon-derivate mit para-substituierter aromatischer amino- oder ethergruppe
CN106573915B (zh) 2014-08-01 2020-12-25 纽韦卢森公司 针对布罗莫结构域有活性的化合物
JP2017525759A (ja) * 2014-08-08 2017-09-07 ダナ−ファーバー キャンサー インスティテュート， インコーポレイテッド ジヒドロプテリジノン誘導体およびその使用
BR112017002369A2 (pt) 2014-08-08 2017-12-05 Dana Farber Cancer Inst Inc derivados de diazepana e usos dos mesmos
TWI712603B (zh) 2014-09-15 2020-12-11 美商英塞特公司 作為ｂｅｔ蛋白抑制劑之三環雜環
EP3206749B1 (de) 2014-10-14 2021-09-08 The Regents of the University of California Die cdk9- und brd4-hemmern flavopiridol und jq1 zur hemmung von knorpelentzündungen
GB201504694D0 (en) 2015-03-19 2015-05-06 Glaxosmithkline Ip Dev Ltd Covalent conjugates
EP3307728A4 (de) 2015-06-12 2019-07-17 Dana Farber Cancer Institute, Inc. Kombinationstherapie von transkriptionshemmern und kinasehemmern
WO2017024406A1 (en) * 2015-08-11 2017-02-16 Neomed Institute N-substituted bicyclic lactams, their preparation and their use as pharmaceuticals
WO2017024408A1 (en) 2015-08-11 2017-02-16 Neomed Institute Aryl-substituted dihydroquinolinones, their preparation and their use as pharmaceuticals
JP6912039B2 (ja) 2015-08-12 2021-07-28 ネオメド インスティテュートＮｅｏｍｅｄ Ｉｎｓｔｉｔｕｔｅ 置換ベンゾイミダゾール、それらの調製及び医薬品としてのそれらの使用
JP2018526421A (ja) 2015-09-11 2018-09-13 ダナ−ファーバー キャンサー インスティテュート， インコーポレイテッド シアノチエノトリアゾロジアゼピンおよびこれらの使用
SG10202007099TA (en) 2015-09-11 2020-08-28 Dana Farber Cancer Inst Inc Acetamide thienotriazoldiazepines and uses thereof
US10501459B2 (en) 2015-10-21 2019-12-10 Neomed Institute Substituted imidazo[1,2-a]pyridines as bromodomain inhibitors
AR106520A1 (es) 2015-10-29 2018-01-24 Incyte Corp Forma sólida amorfa de un inhibidor de proteína bet
EP3380100A4 (de) 2015-11-25 2019-10-02 Dana-Farber Cancer Institute, Inc. Bivalente bromodomänenhemmer und verwendungen davon
WO2017127930A1 (en) 2016-01-28 2017-08-03 Neomed Institute Substituted [1,2,4]triazolo[4,3-a]pyridines, their preparation and their use as pharmaceuticals
DE102017005091A1 (de) 2016-05-30 2017-11-30 Bayer Pharma Aktiengesellschaft Substituierte 3,4-Dihydropyrido[2,3-b]pyrazin-2(1H)-one
PE20190623A1 (es) 2016-06-20 2019-04-26 Incyte Corp Formas solidas cristalinas de un inhibidor de bet
US11833155B2 (en) 2020-06-03 2023-12-05 Incyte Corporation Combination therapy for treatment of myeloproliferative neoplasms
WO2023205251A1 (en) 2022-04-19 2023-10-26 Nuevolution A/S Compounds active towards bromodomains

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1141196A (zh) * 1995-02-27 1997-01-29 拜尔公司 喹喔啉类与蛋白酶抑制剂结合作为药物的应用
US20060019961A1 (en) * 2004-06-09 2006-01-26 Mahaney Paige E Estrogen receptor ligands
CN101573360A (zh) * 2006-10-19 2009-11-04 西格诺药品有限公司 杂芳基化合物、其组合物以及它们作为蛋白激酶抑制剂的用途
TW201109331A (en) * 2009-08-06 2011-03-16 Oncotherapy Science Inc Pyridine and pyrimidine derivatives having ttk-inhibiting activity

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP5913292B2 (ja) * 2010-05-14 2016-04-27 ダナ−ファーバー キャンサー インスティテュート， インコーポレイテッド 代謝を調節する組成物および方法
CN105229002A (zh) * 2012-12-20 2016-01-06 拜耳医药股份有限公司 抑制bet蛋白的二氢吡啶并吡嗪酮

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1141196A (zh) * 1995-02-27 1997-01-29 拜尔公司 喹喔啉类与蛋白酶抑制剂结合作为药物的应用
US20060019961A1 (en) * 2004-06-09 2006-01-26 Mahaney Paige E Estrogen receptor ligands
CN101573360A (zh) * 2006-10-19 2009-11-04 西格诺药品有限公司 杂芳基化合物、其组合物以及它们作为蛋白激酶抑制剂的用途
TW201109331A (en) * 2009-08-06 2011-03-16 Oncotherapy Science Inc Pyridine and pyrimidine derivatives having ttk-inhibiting activity

Cited By (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN109350616A (zh) * 2018-12-18 2019-02-19 南华大学 I-brd9或其衍生物在制备抗癫痫药物中的应用
CN109350616B (zh) * 2018-12-18 2020-04-21 南华大学 I-brd9或其衍生物在制备抗癫痫药物中的应用
US11304935B2 (en) 2018-12-18 2022-04-19 University of South China Use of I-BRD9 or derivatives thereof in preparing anti-epileptic drugs
CN113717080A (zh) * 2021-10-09 2021-11-30 西安瑞联新材料股份有限公司 一种4-氯-2-氰基苯磺酰氯的合成方法

Also Published As

Publication number Publication date
UY35205A (es) 2014-07-31
US20160193206A1 (en) 2016-07-07
WO2014095774A1 (de) 2014-06-26
EP2935260A1 (de) 2015-10-28
TW201427981A (zh) 2014-07-16
HK1213899A1 (zh) 2016-07-15
CA2895404A1 (en) 2014-06-26
JP2016504990A (ja) 2016-02-18
AR094148A1 (es) 2015-07-15

Similar Documents

Publication Publication Date Title
CN105229002A (zh) 抑制bet蛋白的二氢吡啶并吡嗪酮
CN103370318B (zh) 取代的咪唑并哒嗪
CN102762557B (zh) 三唑并吡啶
CN103814029B (zh) 取代的咪唑并哒嗪
CN103687858B (zh) 作为mknk1激酶抑制剂的氨基取代的咪唑并哒嗪
CN103608350B (zh) 三唑并吡啶类化合物
CN104995190A (zh) Bet蛋白抑制剂二氢喹喔啉酮
CN103443100B (zh) 在过度增殖性病症的治疗中用作mps-1和tkk抑制剂的取代的6-咪唑并吡嗪
CN102753547B (zh) 三唑并吡啶衍生物
CN102971321B (zh) 咪唑并吡嗪
CN104114559B (zh) 氨基取代的咪唑并哒嗪
CN105164135A (zh) 4-取代的吡咯并二氮杂卓和吡唑并二氮杂卓
CN105555786A (zh) 作为BET蛋白和极体样激酶的双重抑制剂的取代的二氢吡啶并[3,4-b]吡嗪酮
CN103038235B (zh) 取代的咪唑并吡嗪
CN105492436A (zh) 取代的苯基-2,3-苯并二氮杂环庚三烯
CN103764656A (zh) 杂环基氨基咪唑并哒嗪
CN105189514A (zh) 作为bet-蛋白抑制剂用于治疗过度增殖性疾病的吡咯并-和吡唑并-三唑并二氮杂卓
CN103717604A (zh) 取代的氨基咪唑并哒嗪
CN104781259A (zh) 抑制bet蛋白的5-芳基三唑并氮杂*
CN105518001A (zh) Bet蛋白抑制性的改性的二氢喹喔啉酮类化合物和二氢吡啶并吡嗪酮类化合物
CN103827120A (zh) 6H-噻吩并[3,2-f][1,2,4]三唑并[4,3-a][1,4]二氮杂*
CN103429592A (zh) 作为mps-1和tkk抑制剂用于治疗过度增殖性病症的6-取代的咪唑并吡嗪
CN103429591A (zh) 在治疗过度增殖性病症中用作mps-1和tkk抑制剂的6-取代的咪唑并吡嗪
CN104797585A (zh) 氨基咪唑并哒嗪
CN103958515A (zh) 氨基取代的咪唑并哒嗪

Legal Events

Date Code Title Description
C06 Publication
PB01 Publication
C10 Entry into substantive examination
SE01 Entry into force of request for substantive examination
REG Reference to a national code

Ref country code: HK

Ref legal event code: DE

Ref document number: 1213899

Country of ref document: HK

WD01 Invention patent application deemed withdrawn after publication

Application publication date: 20160106

WD01 Invention patent application deemed withdrawn after publication
REG Reference to a national code

Ref country code: HK

Ref legal event code: WD

Ref document number: 1213899

Country of ref document: HK